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. 2010 Dec;10(10):753–768. doi: 10.2174/187152010794728639

Table 3.

Biological Activity (IC50) of N-Methylated Cyclic Peptides and Standard Peptides in Inhibiting the Binding of Vn and Fg to Isolated Integrins αvβ3 and αIIbβ3, Respectively

Peptide IC50 (µM) αvβ3 IC50 (µM) αIIbβ3 Selectivity αIIbβ3/αvβ3
GRGDSPK 0.21 1.7 8.1
c(RGDfV) 0.0025 1.7 680
1, c(-N(Me)R-GDfV) 0.0055 5.2 945
2, c(R-N(Me)G-DfV) 0.045 > 10 n.c.
3, c(RG-N(Me)D-fV) 0.56 > 10 n.c.
4, c(RGD-N(Me)f-V) 1.4 > 10 n.c.
5, c(RGDf-N(Me)V-) 0.00058 0.86 1483

The selectivity for these receptors is expressed as the ratio between the IC50 values for each integrin subtype [16].